The effect of Henna (Lawsonia inermis) vaginal suppository combined with antibiotic therapy in the treatment of cervicitis: An RCT.

Background: Cervicitis is a prevalent gynecologic disease, which does not usually respond to conventional treatments. Long-term cervicitis can cause serious health problems such as inflammation, infertility, and cancer. Henna oil, an herbal product in Persian medicine, is recommended for uterine diseases like cervicitis. Objective: This study aims to evaluate the efficacy of Henna oil as a vaginal suppository in combination with an antibiotic regimen in the treatment of cervicitis. Materials and Methods: This randomized placebo-controlled trial, included 92 non-menopausal women with cervicitis at the Baqaipur Clinic of Shahid Sadoughi hospital in Yazd and the Persian Medicine Health Center in Ardakan, Yazd, Iran. Participants were further divided into either the Henna oil vaginal suppository group or the placebo group (n = 46/each group). During the study, the antibiotic treatment was administered to both groups. Cervicitis symptoms were compared between the groups and within each group. Results: Of 92 included individuals, 41 in each group completed the study. Results revealed that significant differences were observed in some outcomes, including vaginal discharge (p < 0.001), cervical ulcer size (p < 0.001), dyspareunia (p = 0.046), and postcoital bleeding (p < 0.001), indicating that the treatment was more effective in the henna group compared to the placebo group. Conclusion: Findings supported that the vaginal suppository of Henna oil in combination with antibiotic therapy could be effective in the improvement of clinical symptoms of cervicitis regardless of its pathology.

Traditional Chinese Medicine Erhuang Suppository for Treatment of Persistent High-risk Human Papillomavirus Infection and Its Impact on Transcriptome of Uterine Cervix.

OBJECTIVE: High-risk human papillomavirus (HR-HPV) infection is the chief cause of cervical intraepithelial neoplasia (CIN) and cervical carcinoma. The Erhuang suppository (EHS) is a traditional Chinese medicine (TCM) prepared from realgar (As2S2), Coptidis rhizoma, alumen, and borneolum syntheticum and has been used for antiviral and antitumor purposes. However, whether EHS can efficiently alleviate HR-HPV infection remains unclear. This study was conducted to evaluate the efficacy of EHS for the treatment of persistent HR-HPV infection in the uterine cervix. METHODS: In this study, we evaluated the therapeutic efficacy of EHS in a randomized controlled clinical trial with a 3-month follow-up. Totally, 70 patients with persistent HR-HPV infection were randomly assigned to receive intravaginal administration of EHS or placebo. HPV DNA, ThinPrep cytologic test (TCT), colposcopy, and safety evaluation were carried out after treatment. Microarray analysis was performed to compare transcriptome profiles before and after EHS treatment. A K14-HPV16 mouse model was generated to confirm the efficiency of EHS. RESULTS: After 3 months, 74.3% (26/35) of the patients in the treatment group were HPV negative, compared to 6.9% (2/29) in the placebo group. High-throughput microarrays revealed distinct transcriptome profiles after treatment. The differentially expressed genes were significantly enriched in complement activation, immune response, and apoptotic processes. The K14-HPV16 mouse model also validated the remarkable efficacy of EHS. CONCLUSION: This study demonstrated that EHS is effective against HR-HPV infection and cervical lesions. Additionally, no obvious systemic toxicity was observed in patients during the trial. The superior efficacy and safety of EHS demonstrated its considerable value as a potential cost-effective drug for the treatment of HPV infection and HPV-related cervical diseases.

Effectiveness and tolerability of rectal ointment and suppositories containing sucralfate for hemorrhoidal symptoms: a prospective, observational study.

BACKGROUND AND AIMS: A high number of topical products are available for the treatment of hemorrhoidal symptoms. Sucralfate-based topical products constitute a new treatment alternative that act as a mechanical barrier to facilitate healing. The aim of this prospective, observational study was to determine patient- and physician-assessed effectiveness and tolerability of rectal ointment and suppositories containing sucralfate for the treatment of hemorrhoidal symptoms in routine clinical practice. METHODS: Adult patients with diagnosed, mild-to-moderate, symptomatic non-bleeding hemorrhoids treated with rectal ointment or suppositories containing sucralfate were enrolled. Patients were administered treatment twice per day for at least 1 week until symptom resolution and/or for a maximum of 4 weeks. The primary endpoint was patient-assessed effectiveness on a modified Symptom Severity Score (mSSS, range 0 to 14). Physician-assessed effectiveness (9 symptoms, 0 to 5 Likert scale), hemorrhoid grade, and patient satisfaction were also determined. RESULTS: Five investigators enrolled 60 patients; mean age was 48.4 ± 16.6 years and 72.4% were female. Pain or pressure sensitivity was reported as the most severe symptom by patients, and pressure sensitivity, discharge, soiling, and prolapse by physicians. Mean patient-assessed mSSS at baseline was 6.6 ± 1.9 and was significantly improved overall and in the ointment and suppository groups individually by -4.6 ± 2.0, -4.4 ± 1.8, and -4.8 ± 2.2, respectively (p < 0.0001). Investigator-assessed mean baseline symptom score was 18.1 ± 3.9 and improved by -7.1 ± 4.5, -6.9 ± 5.4, and -7.3 ± 3.5, respectively (p < 0.0001). Investigator-assessed symptoms of pressure sensitivity, swelling, and discharge were improved to the greatest extent. Hemorrhoid grade was improved in 38% of patients at the end of treatment. Compliance with treatment was 97.4% and patient satisfaction with application and onset of action was high (81.3% and 76.2%, respectively). Both the ointment and suppository were well tolerated. CONCLUSIONS: The effectiveness of topical ointment or suppository containing sucralfate on patient- and investigator-assessed hemorrhoidal symptoms in real-life clinical practice was demonstrated. Patient satisfaction was high and treatments were well tolerated. Larger controlled trials are warranted to confirm the results.

VagiBIOM Lactobacillus suppository improves vaginal health index in perimenopausal women with bacterial vaginosis: a randomized control trial.

Bacterial vaginosis (BV) can cause vaginal dysbiosis that may influence general vaginal health and pregnancy complications. Balancing vaginal microbiome using Lactobacillus spp. may be a new way to prevent and treat mild BV. We conducted a randomized, double-blind, placebo-controlled pilot study aimed at evaluating the effect of the product VagiBIOM, a multi-Lactobacillus vaginal suppository, on peri- and premenopausal women with BV in restoring vaginal pH and overall vaginal health by resetting the vaginal microbiome composition. Sixty-six peri- and premenopausal women with BV symptoms were randomized with a 2:1 ratio to be treated with VagiBIOM or placebo suppositories. Vaginal pH, VAS itching score, total Nugent score, and vaginal health index (VHI) were measured. Vaginal microbiome changes before and after the treatment were analyzed by 16S rRNA sequencing and bioinformatics analysis. After 4 weeks of intervention with VagiBIOM or a placebo, the mean score for vaginal pH, VAS itching, and total Nugent score was significantly decreased from the baseline. Compared to the baseline scores, the VHI scores improved significantly following 28-day intervention (p < 0.001). Our results revealed two Lactobacillus species, L. hamsteri, and L. helveticus, as indicator species occurring differentially in the VagiBIOM-treated group. Furthermore, the regression and species network analyses revealed significant bacterial associations after VagiBIOM treatment. Lactobacillus hamsteri was positively associated with the Nugent score and negatively associated with vaginal pH. L. iners and L. salivarius were positively and inversely associated with VHI. As is typical, Bacteroides fragilis was positively associated with vaginal pH and negatively associated with the Nugent score. Interestingly, the Lactobacillus spp. diversity improved after VagiBIOM treatment. The VagiBIOM suppository treatment for peri- and premenopausal women with BV significantly relieved vaginal itching by decreasing vaginal pH and Nugent scores and improving the overall VHI after 4 weeks' intervention. This effect was primarily the result of VagiBIOM improving vaginal Lactobacillus diversity.Trial Registration ClinicalTrials.gov registration: NCT05060029, first registration 09/28/2021: Title: A Pilot Study to Evaluate the Efficacy and Safety of Lactobacillus Species Suppositories on Vaginal Health and pH.

Qingchang suppositry induced remission in patients with mild-to-moderate ulcerative proctitis: a multicenter, prospective, randomized, parallel-controlled clinical trial.

OBJECTIVE: To evaluate the efficacy and safety of Qingchang suppository (, QCS), a preparation of Chinese herbal medicine, in the induction of remission in patients with mild-to-moderate ulcerative proctitis (UP). METHODS: We performed a multicenter, prospective, randomized, parallel-controlled trial to evaluate the efficacy of QCS induction therapy in 140 adult patients with mild-to-moderate UP and TCM syndrome of dampness-heat in large intestine. The patients were randomized to receive QCS (study group) or Salicylazosulfapyridine (SASP) suppository (control group) one piece each time, twice a day, per anum for 12 weeks. Mayo score and main symptoms score were evaluated at weeks 0, 2, 4, 8 and 12, rectosigmoidscopy was taken at weeks 0, 4, 8 and 12, Geboes score, erythrocyte sedimentation rate (ESR), C-reactive protein (CRP) and safety indexes were assessed at weeks 0 and 12. The primary efficacy endpoint is clinical remission rate, the secondary efficacy endpoints are clinical response rate, mucosa healing rate, Geboes score, the remission rates of the main symptoms, the median day to the remission of the symptom, etc. RESULTS: There were no statistical difference in the clinical remission rates, the clinical response rates, the mucosa healing rates, Geboes score, ESR and CRP between the two groups. The remission rates of tenesmus and anal burning sensation of the study group were significantly higher than those of the control group (76.5% vs 25.0%, P = 0.009; 74.51% vs 29.63%, P = 0.003). The median day to the remission of purulent bloody stool of the study group was significantly less than that of control group [11 (1, 64) vs 19 (2, 67), P = 0.007]. The patients receiving QCS had a significantly higher mucosa healing rate at week 4 than the patients receiving SASP suppository (71.42% vs 52.85%, P = 0.023). No adverse event occurred in the study group while the adverse events incidence of the control group was 5.7% (P = 0.049). CONCLUSIONS: QCS could induce the remission of UP as effectively and safely as SASP suppository, and was superior to SASP suppository in relieving the symptoms of tenesmus, anal burning sensation and purulent bloody stool and the time to reach mucosa healing.

Analysis of the Therapeutic Effect of Hemorrhoids Suppositories Plus Fumigation and Hip Bath with Chinese Medicine on Postoperative Pain and Edema of Patients with Mixed Hemorrhoids / 广州中医药大学学报

Objective To investigate the clinical efficacy of hemorrhoids suppositories plus fumigation and hip bath with Chinese medicine on postoperative pain and edema of patients with mixed hemorrhoids.Methods A total of 62 cases of mixed hemorrhoids to be treated surgically were randomly divided into the trial group and the control group,with 31 cases in each group.Both groups of patients were given the surgery of mixed hemorrhoids(high ligation of hemorrhoids or Milligan-Morgan hemorrhoidectomy)and routine postoperative nursing.Additionally,the control group was treated with rectal hemorrhoids suppository,and the trial group was treated with rectal hemorrhoids suppository plus fumigation and hip bath with Chinese medicines of Carthami Flos,Persicae Semen,Corydalis Rhizoma,Talcum,Toosendan Fructus,Aurantii Fructus,Phellodendri Chinensis Cortex,Myrrha,and Olibanum.The course of treatment for the two groups covered 2 weeks.The changes of pain score and edema score in the two groups were observed before and after treatment,and time for the relief of the symptoms,clinical efficacy and therapeutic satisfaction were also compared.Results(1)After 2 weeks of treatment,the total effective rate of the trial group was 96.77%(30/31),and that of the control group was 80.65%(25/31).The intergroup comparison(tested by chi-square test)showed that the therapeutic efficacy of the trial group was significantly superior to that of the control group,and the difference was statistically significant(P＜0.05).(2)After treatment,the pain scores and edema scores of patients in the two groups were significantly decreased compared with those before treatment(P＜0.05),and the decrease of the scores in the trial group was significantly superior to that in the control group with statistically significant difference(P＜0.01).(3)The time for pain relief and time for edema subsidence in the trial group were significantly shorter than those of the control group,and the differences were statistically significant(P＜0.01).(4)The total satisfaction rate of the trial group was 96.77%(30/31),while that of the control group was 77.42%(24/31).The intergroup comparison(tested by chi-square test)showed that the therapeutic satisfaction of the trial group was significantly superior to that of the control group,and the difference was statistically significant(P＜0.05).Conclusion The therapeutic effect of hemorrhoids suppository plus fumigation and hip bath with Chinese medicine in treating postoperative pain and edema of mixed hemorrhoids is remarkably,and the therapy can effectively improve the degree of edema and pain,promote the recovery of the patients,and improve the patient's therapeutic satisfaction.

Clinical Efficacy of Traditional Chinese Medicine Suppository Combined with Yishen Tongluo Qingkang Decoction in Treatment of Immune Infertility / 中国实验方剂学杂志

ObjectiveTo evaluate the clinical efficacy and safety of traditional Chinese medicine （TCM） suppository combined with Yishen Tongluo Qingkang decoction in the treatment of immune infertility. MethodA total of 116 patients meeting the inclusion criteria of this study were randomly divided into an observation group （58 cases） and a control group （58 cases）. The observation group was treated with TCM suppository combined with Yishen Tongluo Qingkang decoction，and the control group was treated with prednisone acetate tablets. Both groups were treated for 12 weeks and followed up six months after treatment. Semen samples of the patients were collected before and after treatment，and the pregnancy status of their spouses，negative conversion rate of seminal plasma anti-sperm antibody （AsAb），sperm concentration，motility，percentage of forward motile sperm，sperm acrosin activity， and incidence of adverse reactions were compared between the two groups. ResultA total of 104 patients completed the study，including 53 cases in the observation group and 51 cases in the control group. Before treatment，the baseline data of the two groups were balanced. After treatment，the total effective rate of the observation group was 92.45%，which was higher than that of the control group （76.47%）（P<0.05），and the negative conversion rate of AsAb in the observation group was higher than that in the control group，but the difference was not statistically significant. After treatment，the sperm motility， percentage of forward motile sperm， and sperm acrosin activity increased in the two groups（P<0.05），and the sperm concentration in the observation group increased （P<0.05）. There was no significant difference in sperm concentration in the control group. After treatment，the sperm concentration，motility，percentage of forward motile sperm， and acrosin activity in the observation group were better than those in the control group （P<0.05）. During the trial，the incidence of adverse reactions in the observation group was lower than that in the control group （P<0.05）. ConclusionTCM suppository combined with Yishen Tongluo Qingkang decoction can significantly increase the negative conversion rate of AsAb and improve the quality of semen in patients with immune infertility.

Preparation and characterization of vaginal suppository of semisynthetic derivatives of ergot alkaloids cabergoline.

Background: There is evidence that vaginal cabergoline can help to prevent ovarian hyperstimulation syndrome. Therefore, the vaginal suppository may be a good choice because it can be administered directly into the vagina and has no adverse effects on the stomach. In this regard we developed a cabergoline suppository as an alternative to cabergoline tablets. Design-Expert was used to determine the most suitable concentrations of PEG 6000/400, and Tween 80 to obtain a stable suppository. Specific ratios of PEG6000/400 and Tween 80 were entered as factors, and release, melting time, and hardness were evaluated as responses. In addition, the final formulation was evaluated for weight changes, pH, drug content, degradation time, deformation time, in vitro drug release, DSC analysis, infrared spectroscopy, and stability properties. Results: The suppositories were all smooth and white. They all had a weight that averaged less than 5 %. The formulations showed a pH between 6 and 6.5. The active ingredient content ranged between 79.666 ± 8.54 % and 99.67 ± 6.55 %. Suppository stiffness was between 2.74 ± 0.04 and 4.20 ± 0.03. The decomposition time of the suppositories varied between 11.25 ± 0.15 to 20.19 ± 0.08 min. The deformation time was between 26.11 ± 0.06 to 38.59 ± 0.47 min. Cabergoline content was released over 45 min from formulations of F10 (∼46 %), F2 (∼64 %), F6 (∼69 %), F4 (∼79 %), F1 (∼88 %), and F7 (∼93 %). However, other formulations released more than 95 % within 45 min. Conclusions: All variables except melting time significantly affected our responses. In vitro studies have indicated that the optimized cabergoline formula could be an excellent alternative to cabergoline oral formulations.

Clinical Background Factors as Predictors of the Efficacy of 5-Aminosalicylic Acid Suppositories in Patients with Ulcerative Colitis.

Introduction: Although the efficacy of 5-aminosalicylic acid (ASA) suppositories for ulcerative colitis (UC) has been reported in many studies, many studies have also described poor adherence to 5-ASA suppository regimens. We aimed to identify the clinical background factors that influence adherence to 5-ASA suppositories to improve adherence and efficacy of the treatment. Methods: We conducted a retrospective cohort study of 61 patients with active UC who were using 5-ASA suppositories. All patients underwent endoscopy and rectal biopsy for histological diagnosis prior to 5-ASA suppository treatment. The efficacy of 5-ASA suppository treatment was compared in relation to clinical background factors (sex, age, disease duration, disease type, clinical activity, Ulcerative Colitis Endoscopic Index of Severity, histological activity, serum C-reactive protein level, concomitant use of immunomodulators, history of steroid use, and dose of oral 5-ASA). Results: The efficacy of 5-ASA suppositories was significantly related to low Lichtiger Colitis Activity Index (LCAI) scores and proctitis type prior to its use. In terms of sex, females tended to show higher efficacy. Multivariate logistic regression analysis using these three factors showed high predictive value for the efficacy of 5-ASA suppositories (AUC, 0.788; sensitivity, 87.2%; and specificity, 63.7%). Conclusion: This study is the first to extract clinical background factors for predicting the efficacy of 5-ASA suppositories. The use of 5-ASA suppositories in patients who are expected to show efficacy will be effective in improving patient co-operation.

Efficacy and mechanism of Baicao Fuyanqing suppository on mixed vaginitis based on 16S rRNA and metabolomics.

Background: Mixed vaginitis is the infection of the vagina by at least two different pathogens at the same time, both of which contribute to an abnormal vaginal environment leading to signs and symptoms. Baicao Fuyanqing suppository (BCFYQ) is a Miao ethnomedicine, used to treat various vaginitis. The aim of this study was to investigate the efficacy and possible mechanism of BCFYQ in the treatment of mixed vaginitis based on 16S rRNA high-throughput sequencing and metabonomics. Methods: Escherichia coli and Candida albicans were used to establish mixed vaginitis model in SD rats. Three groups of low, medium and high doses (0.18/0.36/0.64 g.kg-1) were established, and administered vaginally once a day for 6 consecutive days. After the last administration, vaginal pH and IL-1ß, IL-2, IL-13 and IgA levels were measured, and the vaginal tissue was examined pathologically. In addition, the vaginal flora was characterised by 16S rRNA, and endogenous metabolites in the vaginal tissue were detected by UHPLC-Q-Exactive MS. Results: Compared with the model group, BCFYQ can reduce the vaginal pH of rats, make it close to the normal group and improve the damaged vaginal epithelial tissue. The results of ELISA showed that BCFYQ decreased the levels of IL-1 ß and IL-2 and increased the levels of IL-13 and IgA (P<0.05). In addition, BCFYQ may increase the abundance of vaginal flora, especially Lactobacillus. The differential metabolite enrichment pathway suggests that the therapeutic mechanism of BCFYQ is mainly related to lipid metabolism and amino acid metabolism. Conclusion: Our research shows that BCFYQ has a good therapeutic effect on mixed vaginitis. It repairs the damaged vaginal mucosa by regulating the vaginal flora and lipid metabolism disorders to improve the local immune function of the vagina and inhibit the growth and reproduction of pathogens.

Mechanism of Qingchang Suppository on repairing the intestinal mucosal barrier in ulcerative colitis.

Ulcerative colitis (UC) is a refractory inflammatory bowel disease, and the outcomes of conventional therapies of UC, including 5-aminosalicylic acid, glucocorticoids, immunosuppressants, and biological agents, are not satisfied with patients and physicians with regard to adverse reactions and financial burden. The abnormality of the intestinal mucosal barrier in the pathogenesis of UC was verified. Qingchang Suppository (QCS) is an herbal preparation and is effective in treating ulcerative proctitis. The mechanism of QCS and its active ingredients have not been concluded especially in mucosal healing. This review elucidated the potential mechanism of QCS from the intestinal mucosal barrier perspective to help exploring future QCS research directions.

Effect of Kangfuxiaomi suppository on pelvic inflammatory disease in rats.

Pelvic inflammatory disease (PID) is commonly encountered in gynecological practice. Kangfuxiaomi suppository, made from the compound extract of Periplaneta Americana, is a Traditional Chinese Medicine remedy widely used for the treatment of gynecological disorders. This study aimed to preliminarily explore the therapeutic effect of Kangfuxiaomi suppository in a rat model of PID established by chemical injury and pathogen infection. The key parameters assessed were vulvar inflammation score, vaginal + uterine organ index, and serum levels of interleukin (IL)- 8; tumor necrosis factor (TNF)-α; C-reactive protein (CRP); superoxide dismutase (SOD); and malondialdehyde (MDA). In addition, levels of IL-6, cyclooxygenase (COX)- 2, and IL-2 in cervical tissues as well as that of IL-1ß and prostaglandin E-2 (PGE2) in uterine tissues were measured. The expression levels of nuclear factor-kappa B (NF-κB) p65 and Toll-like receptor 4 (TLR4) in uterine tissues were detected by immunohistochemical method. After Kangfuxiaomi suppository treatment, the vulva inflammation score and histopathological score of PID rats showed a tendency to decrease. Serum IL-8, TNF-α, CRP, and MDA levels were reduced, while SOD levels were significantly increased. Levels of IL-6, IL-2, and COX-2 in cervical tissues were somewhat decreased, and PGE2 and IL-1ß levels in uterine tissue were significantly decreased. Moreover, the levels of NF-κB p65 and TLR4 protein expression were also decreased. These findings demonstrated the therapeutic effect of Kangfuxiaomi suppository in PID rats. The underlying mechanism may involve enhanced antioxidant capacity and decreased secretion of proinflammatory factors via the NF-κB/TLR4 signaling pathway.

3D printed infliximab suppositories for rectal biologic delivery.

Infliximab is a monoclonal antibody that plays an important role in the management and treatment of chronic inflammatory bowel diseases (IBD). Due to its macromolecular structure, its delivery through the oral route is challenging, limiting its administration to only via the parenteral route. The rectal route offers an alternative way for administering infliximab, allowing it to be localised at the disease site and circumventing its passage across the alimentary canal and thus, maintaining its integrity and bioactivity. Three-dimensional (3D) printing is an advanced production technology that permits the creation of dose-flexible drug products from digital designs. The current study assessed the feasibility of utilising semi-solid extrusion 3D printing for the fabrication of infliximab-loaded suppositories for the local treatment of IBD. Various printing inks composed of Gelucire® (48/16 or 44/14) mixed with coconut oil and/or purified water were investigated. It was shown that following reconstitution in water, the infliximab solution can be directly incorporated into the printing ink of Gelucire® 48/16 and can withstand the extrusion process, resulting in well-defined suppositories. Since water content and temperature are critical for safeguarding infliximab's potency, the effect of changing the composition of the printing inks and printing parameters on infliximab's biologic efficiency was evaluated by measuring its binding capacity (i.e., the amount of infliximab that actively binds to its antigen to exert an effect). Despite drug loading assays showing that infliximab remains intact following printing, it was found that the incorporation of water in isolation results in only ∼65% binding capacity. However, when oil is added to the mixture, infliximab's binding capacity increases up to ∼85%. These promising results demonstrate that 3D printing has the potential to be exploited as a novel platform for fabricating dosage forms containing biopharmaceuticals, avoiding patients' compliance issues observed with injectables and addressing their unmet needs.

Mesalazine hollow suppositories based on 3D printing for treatment of ulcerative colitis.

Mesalazine (MSZ) suppositories are a first-line medication for the localized treatment of ulcerative colitis (UC). However, the frequent defecation of patients with UC influences the retention of the suppository in the rectum and multiple doses have to be applied. Here, a mesalazine hollow suppository (MHS) is developed using three-dimensional (3D) printing. The MHS is composed of an inner supporting spring and an outer MSZ-loaded curved hollow shell. Springs were prepared using fused deposition modeling (FDM) 3D printing with thermoplastic urethane filaments, followed by splitting. The optimal parameters, including elasticity, filament diameter, spring inner diameter, and filament distance, were screened. The shell was prepared by FDM 3D printing utilizing MSZ, polyvinyl alcohol, and polyethylene glycol, which were assembled with springs to obtain FDM 3D-printed MHS (F-MHS); if 3D-printed metal molding was used in preparing shell, mold-formed MHS (M-MHS) was obtained. The F-MHS exhibited faster MSZ release than the M-MHS; therefore, the molding method is preferable. The inserted M-MHS was retained in the rat rectum for 5 h without affecting defecation. M-MHS alleviated tissue damage of UC rats and reduced inflammation with low levels of myeloperoxidase and proinflammatory cytokines. Personalized MHS is a promising medication for the localized treatment of UC.

Pharmacokinetic and metabolite profile of orally administered anemoside B4 in rats with an improved exposure in formulations of rectal suppository.

ETHNOPHARMACOLOGICAL RELEVANCE: Pulsatilla chinensis (Bunge) Regel is a traditional Chinese herbal medicine used to treat intestinal amebiasis, malaria, vaginal trichomoniasis, and bacterial infections. Anemoside B4 (AB4), a pentacyclic triterpenoid saponin, is one of the primary bioactive substances in Pulsatilla chinensis (Bunge) Regel, and gavage administration of AB4 to animals has been demonstrated to exhibit anticancer, anti-inflammatory, and antiviral actions. However, AB4 exposure in plasma is very low after oral administration, and the biotransformation of AB4 in vivo after oral administration remains unknown. AIM OF THE STUDY: The reason for conducting this research was to explore at the metabolite profile of AB4 in rats following oral administration. Additionally, we aimed to develop an appropriate extravascular formulation to increase the exposure and duration of AB4 in vivo. MATERIALS AND METHODS: A well-validated HPLC-QQQ-MS/MS method was used for the quantification of AB4 in plasma and was further applied to evaluate and compare the pharmacokinetic properties of AB4 dissolved in a saline solution and AB4 formulations in a rectal suppository or enteric capsule. Reliable UHPLC coupled to Q-Exactive Plus high-resolution MS was used to identify the metabolites in rat plasma, bile, urine, and faeces. RESULTS: AB4 was extensively metabolized, and a total of 29 metabolites were identified. The primary metabolic routes included deglycosylation, oxidation, dehydrogenation, reduction, sulfation, hydration, acetylation, and glucuronidation. The pharmacokinetic comparison showed that both the rectal suppository and enteric capsule increased the exposures of AB4 and one of its active metabolites, 23-hydroxybetulinic acid (23-HA). Notably, rectal suppositories increased systemic AB4 exposure (AUC0-∞) by approximately 49 and 28 times higher than that of the AB4 saline solution and enteric capsules, respectively. The t1/2 of AB4 was extended to approximately 7 h after rectal administration compared to 2 h after oral administration. CONCLUSION: Overall, our study demonstrated that the mismatched exposure-response relationship of AB4 could result from extensive metabolism in the gastrointestinal and circulatory systems. Thus, a rectal suppository could be an alternative formulation of AB4 to obtain both higher and longer exposure.

Cannabis use preferences in women with myofascial pelvic pain: A cross-sectional study.

Objective: Myofascial tenderness is present in most chronic pelvic pain conditions and causes significant distress to patients. Treatment is challenging and often not curative. Cannabis is often used for self-management of chronic pelvic pain. However, we do not know which concentrations and routes of administration are most acceptable to users. We aimed to investigate patterns and willingness of cannabis product use among both habitual users and non-users with myofascial pelvic pain (MPP), to inform therapeutic development. Study design: We conducted a cross-sectional study of questionnaire responses from female patients with MPP from two tertiary pelvic pain centers. We aimed for a convenience sample of 100 responses with representation from both centers. Inclusion criteria were age over 18 with pelvic floor muscle tenderness on standard gynecologic examination. We collected information on demographics, pelvic pain history, cannabis use status, cannabis use preferences, validated opioid misuse risk assessment, and interest in using gynecologic cannabis products and used descriptive analyses. Results: 77/135 (57 %) questionnaire respondents were cannabis users and 58 (43 %) were non-users. Most users consume cannabis daily, (48.1 %) orally (66.2 %) or by smoking (60.7 %), and rated cannabis as effective at relieving pelvic pain. 37/58 (63.8 %) non-cannabis users responded that they would be willing to use cannabis for pelvic pain. Lack of information and potential adverse effects were the most common reasons for unwillingness to use. Approximately 3 of 4 respondents were willing to try vaginal or vulvar application of cannabis products for pelvic pain. Conclusions: This cross-sectional study describes cannabis use patterns in MPP patients. Topical vulvar and vaginal cannabis products are of strong interest to both cannabis users and non-users and warrant further research.

[Origin, development, and modern application value of Chinese herbal lozenges].

Lozenge is one of the traditional dosage forms of Chinese medicine. It has been recorded in traditional Chinese medical classics of all dynasties since the Eastern Han Dynasty and has been developing and evolving continuously. The unique pharmaceutical methods and application scope are the driving force of its emergence, existence, and development. Up to now, lozenge has been included in the Chinese Pharmacopoeia as an independent dosage form. Lozenge has been endowed with new meaning by modern Chinese medicine pharmaceutics, which is worth tracing origin and exploring value. The present study reviewed the origin and development of lozenge, compared lozenge with other similar dosage forms, analyzed the characteristics of modern and ancient dosage forms of lozenge, and discussed the development prospect and potential of lozenge in combination with the demand development of modern Chinese medicine preparation, so as to provide references for expanding the modern application of lozenge.

Effect of vitamin D vaginal suppository on sexual functioning among postmenopausal women: A three-arm randomized controlled clinical trial.

OBJECTIVE: Vaginal atrophy, the second most common complication of menopause, can lead to sexual dysfunction. This study evaluated the effect of a vitamin D vaginal suppository on sexual functioning in postmenopausal women. METHODS: This three-arm randomized controlled trial was conducted between August 2019 and August 2020. The sample comprised 105 postmenopausal women who were referred to comprehensive health service centers to receive postmenopausal care. The inclusion criteria were as follows: (i) being menopausal for at least 1 year, (ii) being married, (iii) being sexually active, and (iv) having sexual desire. Participants were randomly assigned to three groups for 8 weeks of treatment: intervention (vaginal suppository containing 1,000 units of vitamin D3), placebo (vaginal suppository placebo), or control (no treatment). The main outcome measure was sexual functioning, which was assessed using the Female Sexual Function Scale (FSFI) 4 times during the study (i.e., 1 month before the intervention, immediately after the intervention, 1 month after the intervention, and 2 months after the intervention). RESULTS: Immediately and 1 month after the trial, the intervention group had the highest FSFI score, followed by the placebo group, both of which were significantly higher than those of the control group (P<0.05). At the 2-month follow-up, the intervention and placebo groups had similar FSFI scores (P=0.08), both of which were significantly higher than those in the control group (P=0.001 and P=0.03, respectively). CONCLUSION: Vitamin D vaginal suppositories were more effective at improving sexual functioning among postmenopausal women in the short-term and appeared to prevent aging-related sexual functioning decline in the long term.

Gallic acid ameliorates dextran sulfate sodium-induced ulcerative colitis in mice via inhibiting NLRP3 inflammasome.

Background: Ulcerative colitis (UC) is a chronic recurrent inflammatory bowel disease (IBD). The conventional drugs for UC may induce severe side effects. Herbal medicine is considered as a complementary and alternative choice for UC. Purpose: This study aims to estimate the effect of natural polyphenol gallic acid (GA) on the NLRP3 inflammasome with dextran sulfate sodium (DSS)-induced colitis in mice. Study design: The body weights and symptoms of BALB/c mice were recorded. Histological evaluation, ELISA, q-PCR, immunohistochemistry, and western blotting were carried out to observe the morphology, cytokine contents, mRNA expressions, and protein expressions, respectively. Lipopolysaccharide (LPS)-induced RAW264.7 macrophage was used to probe GA's effect on relative protein expression. Results: GA attenuated weight loss (p < 0.05), relieved symptoms, and ameliorated colonic morphological injury (p < 0.05) in mice with colitis induced by DSS. GA also lowered the contents of TNF-α, IL-1ß, IL-18, IL-33, and IFN-γ in the serum and colon of mice, which were elevated by DSS, downregulated protein, and mRNA expressions of the NLRP3 pathway in the colon tissue. Furthermore, GA downregulated the expressions of NLRP3 (p < 0.05), iNOS (p < 0.01), COX2 (p < 0.01), and P-p65 (p < 0.05), and suppressed NO release (p < 0.001) in LPS-induced RAW264.7 cells. Conclusion: GA ameliorated DSS-induced UC in mice via inhibiting the NLRP3 inflammasome. These findings furnish evidence for the anti-inflammatory effect of herbal medicines containing GA on UC.

Fatal complication caused by laxative suppository agent on pediatric patient with hydrocephalus on ventriculo-peritoneal shunt: a case report.

INTRODUCTION: Laxative suppository agent is oftenly used for patient with constipation due to its effectiveness and rapid onset. However, beside the benefit of the drugs, it could cause several side effects which could lead to life-threatening complication. In this report, we present a rare case of laxative's side effect that leads to fatal complication in pediatric patient with history of hydrocephalus and ventriculo-peritoneal (VP) shunt placement. CASE REPORT: An 11 years old boy admitted with general weakness, low nutrition intake, and constipation for 4 days. Patient had a history of VP shunt surgery at half months old due to congenital hydrocephalus. Abdominal X-ray found colon dilatation and fecal material collection. Laxative suppository agent was given to the patient. An hour after the treatment, patient had an abdominal pain followed by defecation, and 30 min after defecation, patient was unresponsive with irregular breathing followed by cardiac arrest. Code blue was activated and resuscitation was done for about 40 min, and patient did not respond to resuscitation and pronounced dead 2.5 h after drug's administration. DISCUSSION: The pathophysiology of this complication is related with elevated intraabdominal pressure that caused abdominal compartment syndrome (ACS), and this condition could lead to several organ dysfunction such as cardiopulmonary and abdominal organ dysfunction inducing central nervous system impairment through raised intracranial pressure (ICP). Pediatric patient with history of hydrocephalus on VP shunt could have a low brain compliance and very susceptible to fatal complication due to acute raised of ICP. CONCLUSION: Laxative suppository agent on pediatric patient with hydrocephalus on VP shunt could lead to fatal complication through ACS and acute elevated ICP pressure. Oral laxative agent should be chosen in constipated patient with neurologic preexisting condition, and patient should be closely monitored if suppository agent is given.